The role of fulvestrant in endometrial cancer

Expert Opin Drug Metab Toxicol. 2017 May;13(5):537-544. doi: 10.1080/17425255.2016.1244264. Epub 2016 Oct 19.

Abstract

Endometrial cancer is the most common malignancy of the female genital tract in industrialized countries. The traditional treatment of endometrial cancer is based on a surgical approach. In recent years, systemic endocrine therapy has demonstrated good efficacy in recurrent or metastatic setting, delaying progression, ameliorating quality of life and palliating symptoms. Areas covered: Phase I and II studies on selective estrogen receptor down-regulators used for the treatment of endometrial cancer treatment have been reviewed. The pharmacokinetic and pharmacodynamic features of selective receptor down-regulators have been also investigated. Expert opinion: Selective estrogen receptor down-regulators may exhibit clinical efficacy in the treatment of gynecological malignancies due to their pure estrogen receptor antagonist properties. However, up to now data are still limited and some unsolved questions remain. Fulvestrant has poor oral bioavailability and low pharmacodynamic characteristics. Further trials are required to examine new selective estrogen receptor down-regulator agents with better pharmacodynamic and pharmacokinetic profiles.

Keywords: Anti-hormone therapy; SERD; endometrial cancer; fulvestrant; gynecologic oncology; selective estrogen receptor down-regulators.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents, Hormonal / pharmacokinetics
  • Antineoplastic Agents, Hormonal / pharmacology
  • Antineoplastic Agents, Hormonal / therapeutic use*
  • Biological Availability
  • Disease Progression
  • Endometrial Neoplasms / drug therapy*
  • Endometrial Neoplasms / pathology
  • Estradiol / analogs & derivatives*
  • Estradiol / pharmacokinetics
  • Estradiol / pharmacology
  • Estradiol / therapeutic use
  • Estrogen Receptor Antagonists / pharmacokinetics
  • Estrogen Receptor Antagonists / pharmacology
  • Estrogen Receptor Antagonists / therapeutic use
  • Female
  • Fulvestrant
  • Humans
  • Quality of Life

Substances

  • Antineoplastic Agents, Hormonal
  • Estrogen Receptor Antagonists
  • Fulvestrant
  • Estradiol